Chemical Structure : Etoricoxib
CAS No.: 202409-33-4
货号: PC-20873Not For Human Use, Lab Use Only.
Etoricoxib (MK-0663) is a potent, selective and orally active inhibitor of COX-2 with IC50 of 1.1 uM for COX-2 (LPS-induced prostaglandin E2 synthesis), shows no activity against COX-1.
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Etoricoxib (MK-0663) is a potent, selective and orally active inhibitor of COX-2 with IC50 of 1.1 uM for COX-2 (LPS-induced prostaglandin E2 synthesis), shows no activity against COX-1.
Etoricoxib does not inhibit platelet or human recombinant COX-1 under most assay conditions (IC50>100 uM).
Etoricoxib is a potent inhibitor in models of carrageenan-induced paw edema (ID(50) 0.64 mg/kg), carrageenan-induced paw hyperalgesia (ID(50)=0.34 mg/kg), LPS-induced pyresis (ID(50) = 0.88 mg/kg), and adjuvant-induced arthritis (ID(50)=0.6 mg/kg/day) in rats.
Etoricoxib reversed LPS-induced pyresis by 81% within 2 h of administration at a dose of 3 mg/kg and showed no effect in a fecal 51Cr excretion model of gastropathy at 100 mg/kg/day for 5 days.
分子量 | 358.84 | |
分子式 | C18H15ClN2O2S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl) pyridine |
1. Riendeau D, et al. J Pharmacol Exp Ther. 2001 Feb;296(2):558-66.
2. Chauret N, et al. Bioorg Med Chem Lett. 2001 Apr 23;11(8):1059-62.
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